Details of the Drug Formulation (DFM)

General Information of DFM (ID: F05911)
Name
Digoxin 0.1875 mg tablet
Company
Concordia Pharmaceuticals; Covis Pharmaceuticals
Active Pharmaceutical Ingredient (API) Digoxin API Info click to show the detail info of this API
Cardiac arrhythmia ICD-11: BC65 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E08SAL DIG Info D&C green no. 5 Colorant
E00DHW DIG Info Lactose monohydrate Binding agent ...
E01UTP DIG Info Magnesium stearate lubricant
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: P2Y purinoceptor 2 (P2RY2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG D&C green no. 5
                    Biological Activity IC50 = 3930 nM (estimated based on the structural similarity with CHEMBL401859 ) [1]
                    Structural Similarity Tanimoto coefficient = 0.934131737
                    Tested Species Homo sapiens (Human)
                    UniProt ID P2RY2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG D&C green no. 5
                    Biological Activity IC50 = 30000 nM (estimated based on the structural similarity with CHEMBL401859 ) [1]
                    Structural Similarity Tanimoto coefficient = 0.934131737
                    Tested Species Mus musculus (Mouse)
                    UniProt ID P2RY2_MOUSE
            DBT Name: P2Y purinoceptor 4 (P2RY4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG D&C green no. 5
                    Biological Activity IC50 = 1910 nM (estimated based on the structural similarity with CHEMBL401859 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.934131737
                    Tested Species Homo sapiens (Human)
                    UniProt ID P2RY4_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO2B1 (OATPB) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG D&C green no. 5
                    Biological Activity Inhibition ratio = 89 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG D&C green no. 5
                    Biological Activity Ki = 1.54 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
References
1 Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 1; 18(1):223-7.
2 Development of Potent and Selective Antagonists for the UTP-Activated P2Y 4 Receptor. J Med Chem. 2017 Apr 13; 60(7):3020-3038.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.

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